Dapagliflozin

Catalog No.S1548 Synonyms: BMS-512148

Dapagliflozin Chemical Structure

Molecular Weight(MW): 408.87

Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.

Size Price Stock Quantity  
In DMSO USD 280 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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3 Customer Reviews

  • (B) Clonogenic survival of prostate cancer cells treated with Canagliflozin, Dapagliflozin or Salicylate and expressed relative to the vehicle controls.

    Mol Metab, 2016, 5(10):1048-56.. Dapagliflozin purchased from Selleck.

    Mol Cell Endocrinol, 2016, 420:37-45.. Dapagliflozin purchased from Selleck.

  • Mol Cell Biochem,2015, 400(1-2):57-68.. Dapagliflozin purchased from Selleck.

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Notes:

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Biological Activity

Description Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Features More potent stimulator of glucosuria than other SGLT2 inhibitors.
Targets
hSGLT2 [1]
1.1 nM(EC50)
In vitro

Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. [1] Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly selective versus GLUT transporters and displays 8–9% inhibition in protein-free buffer at 20 μM and virtually no inhibition in the presence of 4% bovine serum albumin. [2] Dapagliflozin has good permeability across Caco-2 cell membranes and is a substrate for P-glycoprotein (P-gp) but not a significant P-gp inhibitor. Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM. Dapagliflozin shows no inhibitory responses or induction to human P450 enzymes. The in vitro metabolic pathways Dapagliflozin are glucuronidation, hydroxylation, and O-deethylation. [3]

In vivo Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the metabolic stability conferred by the C-glucoside linkage. Dapagliflozin displays a favorable absorption, distribution, metabolism, and excretion (ADME) profile and is orally bioavailable. [1] Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and increase in urine volume in normal rats over 24 hours post-dose. Dapagliflozin induces increase in urine glucose and urine volume excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats. Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2 weeks of treatment, without any marker of renal or liver toxicity. [2] Dapagliflozin significantly reduces the development of hyperglycaemia, with lowered blood glucose. Dapagliflozin could improve the insulin sensitivity, reduce β-cell mass and the development of impaired pancreatic function. [4]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Normal Sprague Dawley rats or streptozotocin induced male Sprague Dawley rats
  • Formulation: 5% mpyrol, 20% PEG400, and 20 mM sodium diphosphate
  • Dosages: 0.01-10 mg/kg (1 mL/kg) followed by a 50% glucose solution (2 g/kg)
  • Administration: Dosed orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (200.55 mM)
Ethanol 17 mg/mL (41.57 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 408.87
Formula

C21H25ClO6

CAS No. 461432-26-8
Storage powder
in solvent
Synonyms BMS-512148

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03036150 Recruiting Chronic Kidney Disease AstraZeneca February 2017 Phase 3
NCT03036124 Not yet recruiting Chronic Heart Failure With Reduced Ejection Fraction (HFrEF) AstraZeneca February 2017 Phase 3
NCT02987738 Not yet recruiting Type1diabetes Kinderkrankenhaus auf der Bult|AstraZeneca|Alcedis GmbH February 2017 Phase 1
NCT03030235 Not yet recruiting Chronic Heart Failure With Preserved Systolic Function Saint Lukes Health System February 2017 Phase 4
NCT02919345 Not yet recruiting Diabetes Mellitus, Type 2|Coronary Artery Disease|Carotid Artery Diseases University of Campinas, Brazil|AstraZeneca January 2017 Phase 4
NCT02981966 Not yet recruiting Diabetes Mellitus, Type 2 The University of Texas Health Science Center at San Antonio|AstraZeneca January 2017 Phase 4

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SGLT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID